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Vesicular Drug Delivery-An Novel Approach S. Umadevi et al, Indo American Journal of Pharmaceutical Research, 2012:2(8) ISSN NO: 2231-6876 Indo American Journal of Pharmaceutical Research. 2012:2(8) INDO AMERICAN Journal home page: JOURNAL OF http://www.iajpr.com/index.php/en/ PHARMACEUTICAL RESEARCH A review;Vesicular drug delivery-an novel approach S. Umadevi*, K. Sasidharan, K. Nithyapriya, R.Venkatanarayanan Department of Pharmaceutics, RVS College of Pharmaceutical Sciences, Sulur, Coimbatore-641402. India ARTICLE INFO ABSTRACT Article history Novel drug delivery system aims to provide some control in temporal Received 25 July 2012 or spatial nature of the drug release in the body. In recent years, Available online 30 July 2012 vesicle have been the vehicle of choice in drug delivery for targeting and controlled release and it can solve the problems of drug solubility, instability and rapid degradation. Vesicular drug delivery Keywords reduces cost of the therapy and can incorporate both the hydrophilic Vesicular system, and lipophilic drugs. Nowadays, a number of vesicular drug delivery bioavailability, system such as liposome, pharmacosomes, ethosomes, depot, controlled transferosomes etc. was developed. This article reviews different release. aspects of this vesicular drug delivery system including their preparation, characterization, advantages and their applications in the drug delivery. Corresponding author Department of pharmaceutics, Faculty of pharmacy,RVS College of Pharmaceutical Sciences, Sulur, Coimbatore, Pin – 641402, Tamilnadu, India. Email ID:[email protected] Phone No:+91 9444132145 Please cite this article in press as: S. Umadevi, A review;Vesicular drug delivery-an novel approach . Indo American Journal of Pharm Research. 2012:2(8). 833 S. Umadevi et al, Indo American Journal of Pharmaceutical Research, 2012:2(8) ISSN NO: 2231-6876 INTRODUCTION A number of technical advancement has been recently made in developing new techniques for drug delivery. These techniques are capable of regulating the rate of drug delivery, sustaining the duration of therapeutic action or targeting the delivery of drug to a tissue. This advancement has already leads to development of several novel drug delivery systems. At present, no available drug delivery system behaves ideally, but many attempts have been made to achieve them through various novel approaches in drug delivery. The main aim of novel drug delivery system is to provide some control of drug release in the body, which is either of temporal or spatial nature or both. The following are the some advantages of novel drug delivery system: Controlled administration of therapeutic dose at desirable delivery rate, maximization of efficiency dose relationship, reduction of adverse side effects and enhancement of patient compliance. The novel drug delivery system should possess two characteristics: One is the delivery of drug at a determined rate and second is the release of the drug at the site of action. There are different types of pharmaceutical carriers are present.1 They are particulate type carrier (lipid particles), microspheres, nanoparticles, polymeric micelles and vesicular system (liposomes, transferosomes, pharmacosomes, ethosomes, niosomes etc.).2,3,4,5 Nowadays vesicles as a carrier system have been become the vehicle of choice for the drug delivery and lipid vesicles were found to be of value in immunology, membrane biology and diagnostic technique and most recently in genetic engineering.6 Vesicular systems The vesicular systems are highly ordered assembles of one are concentric lipid bilayer formed when certain amphiphilic building blocks are confronted with water. These biological vesicles origin was first reported in 1965 by Bingham. The lipid vesicles are rationalized for topical application since,7 • The lipids, because of their lipophilic nature may serve as organic phase for poorly aqueous soluble substances.7 • They can be targeted intracellular and due to lipophilic nature, it acts as penetration enhancer.8 • Vesicular drug delivery reduces the cost of therapy by improved bioavailability of medication. • These carriers play an increasing important role in drug delivery because of the reduction in drug release rate; it is possible to reduce the toxicity of drug case of poorly soluble drugs. They can incorporate both by hydrophilic and lipophilic drugs. • Prolong the existence of the drug in systemic circulation and reduces the toxicity. Delays elimination of rapidly metabolized drugs and thus function as sustained release systems.9 Types of vesicular drug delivery carriers7 There are different types of vesicular drug delivery system. They are as follows: Liposomes: Liposomes are simple microscopic vesicles in which an aqueous volume is entirely enclosed by a membrane composed of a lipid molecule. These are the most widely known vesicular delivery system. The assembly into closed bilayered structures is a spontaneous process and usually needs some input of energy in the form of physical agitation, sonication, heat etc. The lipid soluble or lipophilic drugs get entrapped within the bilayered membrane, whereas water soluble or hydrophilic drugs get entrapped in the central aqueous core of the vesicles. It has wide advantages of biodegradability, moisturizing, restoring action and sustained dermal release. 10 834 S. Umadevi et al, Indo American Journal of Pharmaceutical Research, 2012:2(8) ISSN NO: 2231-6876 Pharmacosomes: “Pharmakon” means linking a drug and “soma” means carrier. They are the colloidal dispersions of drug covalently bound to lipids. Pharmacosomes are amphiphilic lipid vesicular system containing phospholipids complex which reduces interfacial tension and at higher concentration exhibit mesomorphic behaviour. Any drug possessing an active hydrogen atom (- COOH,-OH,-NH2 etc.) can be esterified to the lipid with or without spacer chain that strongly result in an amphiphilic compound which will facilitate membrane, tissue or cell wall transfer in the organism. It improves bioavailability of poorly water soluble drug as well as poorly lipophilic drug.11 Transferosomes: Transferosomes are vesicles composed of phospholipids with surfactant and ethanol as well as ultradeformable vesicle possessing an aqueous core surrounded by the complex lipid bilayer. Higher membrane hydrophilicity and flexibility of transferosomes tend to avoid aggregation and fusion. Transferosomes was introduced for the effective transdermal delivery of number of low and high molecular weight drugs.12 It can penetrate the intact stratum corneum spontaneously along two routes in the intracellular lipid that differ in their bilayers properties. It consists of both hydrophilic and hydrophobic properties; high deformability gives better penetration of intact vesicles.13 Ethosomes: Ethosomes are lipid vesicles containing phospholipids, alcohol (ethanol and isopropyl alcohol) in high concentration and water. These are the slight modification of well established drug carrier liposomes. Ethosomes are noninvasive delivery carriers that enable drugs to reach the deep skin layers and or the systemic circulation. Unlike classic liposomes, that are known mainly to deliver drugs to the outer layers of skin, Ethosomes can permeate through the stratum corneum barrier.14 It can entrap drug molecules with various physicochemical characteristics like hydrophilic, lipophilic or amphiphilic. Niosomes: Niosomes are non-ionic surfactant vesicles obtained on hydration of synthetic non-ionic surfactants with or without incorporation of cholesterol or other lipids. The vesicle is composed of a bilayer of non-ionic surface active agents and hence, it was named as niosomes.15 Niosomes have recently been shown to greatly increase transdermal drug delivery and also can be used in targeted drug delivery. They improve oral bioavailability of poorly absorbed drugs and enhance skin penetration.16 Vesosomes: Bilayer compartments led to the development of a multicompartment structure of unilamellar vesicles trapped within an exterior membrane called vesosome. The inner compartments of the vesosome can encapsulate multiple drugs or have different bilayer compositions to optimize release.17 Phytosomes: Phytosomes are complexes between a pure phospholipid and pure active principles from the chemical perspective. Phytosomes are developed to incorporate standardized plant extract or water soluble phytoconstituents into phospholipids to produce lipid compatible molecular complexes called phytosomes.18,19 835 S. Umadevi et al, Indo American Journal of Pharmaceutical Research, 2012:2(8) ISSN NO: 2231-6876 Table No.1 List of drug Available in lipid vesicular delivery system Drug Carrier Insulin Liposomes Didanosine Pharmacosomes Acyclovir Pindolol maleate Pharmacosomes Bupranolol HCl Norgesterol Transferosomes Tamoxifen Interferon α Transferosomes nterleukin Doxorubicin Niosomes Methotrexate Pentoxifylline Niosomes Diclofenac Minoxidil Ethosomes Testosterone Sphingosomes: These are concentric, bilayered vesicle in which an aqueous volume is entirely enclosed by a membranous lipid bilayer mainly composed of natural or synthetic sphingolipid.20 Liposomal phospholipid can either undergo chemical degradation such as oxidation and hydrolysis or as a result of these changes, liposome maintained in aqueous suspension may aggregrate, fuse or leak their content. The hydrolysis may be avoided altogether by use of lipid which contains ether or amide linkage instead of ester linkage (Sphingolipid) or phospholipid derivatives with the 2-ester linkage
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